Bazedoxifene hydrochloride NEW
| Price | $55 | $140 | $252 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-09 |
Product Details
| Product Name: Bazedoxifene hydrochloride | CAS No.: 198480-56-7 |
| Purity: 98.74% | Supply Ability: 10g |
| Release date: 2024/11/09 |
Product Introduction
Bioactivity
| 名稱 | Bazedoxifene hydrochloride |
| 描述 | Bazedoxifene hydrochloride (TSE 424 hydrochloride) is an orally active, selective, and potent estrogen receptor modulator (SERM) that crosses the blood-brain barrier and is an inhibitor of IL-6/GP130 protein interactions with high affinity for ERα and ERβ. It has a high affinity for ERα and ERβ and can be used to study postmenopausal osteoporosis and vasodilator-related diseases. |
| 細(xì)胞實(shí)驗(yàn) | For the proliferation assay, cells are plated at 20,000 cells/well in a 24-well plate in DMEM/F12 (50:50) (phenol red-free) with 10% charcoal/dextran-treated FBS and 1 × GlutaMAX-1. After overnight incubation, the medium is aspirated and treatments in DMEM/F12 (50:50) (phenol red-free) with 2% charcoal/dextran-treated FBS and 1 × GlutaMAX-1 are added to the wells. Each plate has a vehicle (baseline proliferation) and treatments. Treatments included 10 pM 17β-estradiol determined to be the EC80 for 17β-estradiol and 17β-estradiol in combination with six concentrations of BZA. Treatments from d 1 are renewed on d 3 and d 6 by aspirating medium from wells and replacing with fresh medium and treatments. On d 7, cells are detached from the plate using trypsin-EDTA and counted using a Multisizer II.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Ligand binding competition experiments: Test compounds are initially solubilized in DMSO and the final concentration of DMSO in the binding assay is ≤ 1%. Eight dilutions of each test compound are used as an unlabelled competitor for [3H]17β-estradiol. Typically, a set of compound dilutions would be tested simultaneously on human, rat and mouse ER-α and ER-β. The results are plotted as measured DPM vs. concentration of test compound. For dose-response curve fitting, a four parameter logistic model on the transformed, weighted data are fit and the IC50 is defined as the concentration of compound decreasing maximum [3H]estradiol binding by 50%. For active compounds, the IC50 is determined at least three times. It should be noted that IC50 values are not direct measures of a ligand's affinity for the receptor. Rather, they can only be compared as relative values, in this case to 17β-estradiol. |
| 體外活性 | In AsPC-1 cells, Bazedoxifene hydrochloride (at concentrations of 10 μM and 20 μM; treated for 2 hours) is able to inhibit STAT3 phosphorylation induced by IL-6, IL-11, or OSM (each at 50 ng/mL)[2]. |
| 體內(nèi)活性 | In 6-week-old female athymic nude mice, Bazedoxifene hydrochloride ( 5 mg/kg ; oral gavage, daily, for 18 days ) was used to Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells[2]. |
| 存儲(chǔ)條件 | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : <1 mg/mL Ethanol : <1 mg/mL DMSO : 93 mg/mL (183.4 mM) |
| 關(guān)鍵字 | TSE-424 | TSE424 | TSE 424 | STAT3 | SERM | selective | receptor | protein-protein | modulator | interactions | IL-6/GP130 | Estrogen Receptor/ERR | estrogen | ERβ | ERα | Bazedoxifene HCl | Bazedoxifene |
| 相關(guān)產(chǎn)品 | Sodium Thiocyanate | Disulfiram | Inosine pranobex | Kaempferol | Tamoxifen | Amlexanox | Mifepristone | Estradiol | Dexamethasone | Melatonin | Diallyl disulfide | Ethisterone |
| 相關(guān)庫(kù) | FDA上市及藥典收錄分子庫(kù) | 經(jīng)典已知活性庫(kù) | 上市藥物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | FDA 上市藥物庫(kù) | 口服活性化合物庫(kù) | 免疫/炎癥分子化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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